ABSTRACT Because tumor cells can survive chemo/radiation therapies through DNA repairment mediated by poly(ADP- ribose) polymerase-1 (PARP-1), PARP-1 inhibitors (PARPis) alone, or in combination with chemotherapy or radiation therapy, have led to substantial gains in the overall survival of cancer patients, by obstructing single strand DNA repair. With multiple ongoing clinical trials using PARPis to treat glioma, to assess baseline PARP expression levels through quantitative PARP PET imaging will provide prognostic information. However, none of the current PARP imaging agents under development is brain penetrant, making the reliable quantification of PARP-1 in brain challenging. Herein, we propose to evaluate a brain penetrant PARP-1 inhibitor and its analogs as potential PET imaging agents.